大鼠大脑皮层[3H]地西帕明结合的药理学特征

Pavel D. Hrdina
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引用次数: 9

摘要

1.1. [3H]地西帕明与大鼠大脑皮层膜的特异性结合是双相的,数据的Scatchard分析显示了两个不同的成分:高亲和力成分,解离常数(KD)为4.5 nM,低亲和力成分(KD = 80 nM)。2.2。不同的化合物在取代高亲和力的[3H]地西帕明和[3H]丙咪嗪结合方面表现出不同的效力顺序。去甲替林和尼西汀是[3H]地西帕明特异性结合的最有效替代物,而氯丙帕明和氟西汀在[3H]地西帕明结合位点的竞争中表现出最强的效力。各种药物抑制[3H]去西帕明结合的能力与其阻断脑内神经元摄取去甲肾上腺素的能力有显著相关性。4.4。结果表明,[3H]地西帕明的高亲和力结合与[3H]丙咪嗪不同,并且最有可能与神经元摄取去甲肾上腺素的部位有关。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmacological characterization of [3H] desipramine binding in rat cerebral cortex

  • 1.

    1. The specific binding of [3H]desipramine to membranes from rat brain cortex is biphasic and the Scatchard analysis of data shows two distinct components: the high affinity component, with a dissociation constant (KD) of 4.5 nM and the low affinity component (KD = 80 nM).

  • 2.

    2. Different order of potency in displacing the high affinity [3H]desipramine and [3H]imipramine binding was shown by various compounds tested. Nortriptyline and nisoxetine were the most potent displacers of [3H]desipramine specific binding while chlorimipramine and fluoxetine showed highest potency in competing for [3H]imipramine binding sites.

  • 3.

    3. Significant correlation was found between the ability of various drugs to inhibit [3H]desipramine binding and their potency to block the neuronal uptake of noradrenaline in brain.

  • 4.

    4. The results suggest that the high affinity binding of [3H]desipramine is distinct from that of [3H]imipramine and is most likely associated with sites involved in neuronal uptake of noradrenaline.

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